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Preparation method of sitagliptin intermediate

A sitagliptin and intermediate technology, applied in the field of organic compound synthesis and pharmaceuticals, can solve the problems of troublesome solvent recovery and low product yield, and achieve the effects of reducing production costs, improving production efficiency, and good social and economic benefits

Pending Publication Date: 2020-06-30
HUNAN FURUI BIOPHARMA TECH CO LTD
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  • Abstract
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Problems solved by technology

[0007] It can be known from the above reaction formula that in the existing synthetic method of sitagliptin intermediate, more solvents are used in the whole preparation process, the final product yield is low, and the recovery and treatment of the solvent is troublesome in the follow-up. The synthesis process is optimized to increase production efficiency

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  • Preparation method of sitagliptin intermediate
  • Preparation method of sitagliptin intermediate
  • Preparation method of sitagliptin intermediate

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Embodiment Construction

[0023] The technical solutions of the present invention will be clearly and completely described below in conjunction with the embodiments of the present invention. Obviously, the described embodiments are only some of the embodiments of the present invention, rather than all of them. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without creative efforts fall within the protection scope of the present invention.

[0024] The preparation method of a kind of sitagliptin intermediate shown as embodiment, synthetic route is:

[0025]

[0026] Its preparation method, under the protection of nitrogen, under acidic conditions, using ethyl acetate as the reaction solvent, the reaction temperature is between 55 ~ 80 ° C, the compound 1 is converted into the compound 2, and the suspension containing the compound 2 is obtained; the compound The ratio of 1 to ethyl acetate is controlled within the range of 1g:5...

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Abstract

The invention provides a method for preparing a sitagliptin intermediate, which comprises the following steps of: converting a compound 1 into a compound 2 at the reaction temperature of 55 to 80 DEGC by taking ethyl acetate as a reaction solvent under the protection of nitrogen and under an acidic condition to obtain turbid liquid containing the compound 2, wherein the ratio of the compound 1 toethyl acetate is controlled to be 1g:5-10ml. According to the present invention, with the method, the defects of the existing process are improved, the production efficiency is improved, the production cost is reduced, the good social benefits and the good economic benefits can be provided, and the economic value potential is large.

Description

technical field [0001] The present invention relates to the technical field of organic compound synthesis and pharmacy, more specifically, relate to the preparation method of a kind of sitagliptin intermediate that is used to prepare diabetes treatment medicine especially. Background technique [0002] Sitagliptin (sitagliptin) is a new type of anti-type 2 diabetes drug developed by Merck in the United States. It is the first dipeptidyl peptidase-4 (DPP-4) inhibitor drug for the treatment of type 2 diabetes. In October 2006, it was approved for marketing by the US FDA. The mechanism of sitagliptin is different from that of previous oral hypoglycemic drugs. Existing clinical experiment data show that sitagliptin alone or in combination with metformin and pioglitazone has a significant hypoglycemic effect. The risk is very low and it does not cause weight gain. [0003] 3-(Trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydrochloride is an important compou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04
CPCC07D487/04
Inventor 鲁光英周跃辉
Owner HUNAN FURUI BIOPHARMA TECH CO LTD
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